Development of Selective Nitrile Inhibitors and ‘Activity-Based’ Probes For Human Cathepsins K and S
Development of Selective Nitrile Inhibitors and ‘Activity-Based’ Probes For Human Cathepsins K and S
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DissertationDate of Exam
14.05.2012Date of Publication
20.06.2012Advisor
Gütschow, MichaelCo-Referee
Müller, Christa E.Metadata
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Abstract
Cysteine cathepsins show a high degree of similarity and play a significant role in many (patho)physiological processes such as bone remodeling, antigen presentation, osteoporosis, autoimmune disorders, and cancer. Therefore, cathepsins represent important targets for the development of new therapeutics and diagnostic tools. Inhibitors of cysteine cathepsins are mainly peptidic or peptidomimetic structures containing electrophilic groups prone to covalent interactions with the active-site cysteine. Among them, nitrile-based inhibitors receive the most attention in current drug discovery. The development of potent and selective nitrile inhibitors and fluorescent 'activity-based' probes for human cathepsins K and S is described in this dissertation.
Subjects
Cysteine cathepsins, cathepsin K, cathepsin S, bone remodeling, antigen presentation, osteoporosis, autoimmunity, dipeptide nitriles, azadipeptide nitriles, fluorescent 'activity-based' probes
Classification (DDC)
500 Naturwissenschaften 540 Chemie 610 Medizin, GesundheitFrizler, Maxim: Development of Selective Nitrile Inhibitors and ‘Activity-Based’ Probes For Human Cathepsins K and S. - Bonn, 2012. - Dissertation, Rheinische Friedrich-Wilhelms-Universität Bonn.
Online-Ausgabe in bonndoc: https://nbn-resolving.org/urn:nbn:de:hbz:5n-28908
Online-Ausgabe in bonndoc: https://nbn-resolving.org/urn:nbn:de:hbz:5n-28908
@phdthesis{handle:20.500.11811/5325,
urn: https://nbn-resolving.org/urn:nbn:de:hbz:5n-28908,
author = {{Maxim Frizler}},
title = {Development of Selective Nitrile Inhibitors and ‘Activity-Based’ Probes For Human Cathepsins K and S},
school = {Rheinische Friedrich-Wilhelms-Universität Bonn},
year = 2012,
month = jun,
note = {Cysteine cathepsins show a high degree of similarity and play a significant role in many (patho)physiological processes such as bone remodeling, antigen presentation, osteoporosis, autoimmune disorders, and cancer. Therefore, cathepsins represent important targets for the development of new therapeutics and diagnostic tools. Inhibitors of cysteine cathepsins are mainly peptidic or peptidomimetic structures containing electrophilic groups prone to covalent interactions with the active-site cysteine. Among them, nitrile-based inhibitors receive the most attention in current drug discovery. The development of potent and selective nitrile inhibitors and fluorescent 'activity-based' probes for human cathepsins K and S is described in this dissertation.},
url = {https://hdl.handle.net/20.500.11811/5325}
}
urn: https://nbn-resolving.org/urn:nbn:de:hbz:5n-28908,
author = {{Maxim Frizler}},
title = {Development of Selective Nitrile Inhibitors and ‘Activity-Based’ Probes For Human Cathepsins K and S},
school = {Rheinische Friedrich-Wilhelms-Universität Bonn},
year = 2012,
month = jun,
note = {Cysteine cathepsins show a high degree of similarity and play a significant role in many (patho)physiological processes such as bone remodeling, antigen presentation, osteoporosis, autoimmune disorders, and cancer. Therefore, cathepsins represent important targets for the development of new therapeutics and diagnostic tools. Inhibitors of cysteine cathepsins are mainly peptidic or peptidomimetic structures containing electrophilic groups prone to covalent interactions with the active-site cysteine. Among them, nitrile-based inhibitors receive the most attention in current drug discovery. The development of potent and selective nitrile inhibitors and fluorescent 'activity-based' probes for human cathepsins K and S is described in this dissertation.},
url = {https://hdl.handle.net/20.500.11811/5325}
}
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